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AZD7507

Catalog No.GC19404

AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity)

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AZD7507 Chemical Structure

Cas No.: 1041852-85-0

Size Price Stock Qty
5mg
$171.00
In stock
25mg
$342.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

Mice[2]Male CD1 nude mice are injected subcutaneously with 5 × 105 human ICC cells from human cell line WITT-1, CC-LP-1, or SNU-1079 (n = 24 in all cases) suspended in culture media/RGF Matrigel (Gibco) mix (1:1). Cells are engrafted bilaterally in the flank and allowed to form tumors over 3 weeks. Once palpable tumors have formed, mice are randomized into 3 groups using GraphPad online software. Xenografted mice are injected with liposomal clodronate at 4 μL/g intravenously. The control for this treatment is saline alone or liposomes not containing clodronate (both given at 4 μL/g intravenously). All of these treatments are given every 48 hours for 3 weeks. CSFR1 inhibitors AZD7507 and GW2580 are made up in sterile water containing 0.5% methylcellulose and 0.1% Tween-80. AZD7507 is given twice daily at 100 mg/kg, whereas GW2580 is given daily at 160 mg/kg. Control animals are given water containing 0.5% methylcellulose and 0.1% Tween-80. ICG-001 (5 mg/kg) or C-59 (20 mg/kg) is given by intraperitoneal injection. The vehicle for this is physiological saline. Control animals are given vehicle alone. In all cases inhibitors and vehicle are given 3 times per week[2].

References:

[1]. Scott DA, et al. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6.
[2]. Boulter L, et al. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. Send to J Clin Invest. 2015 Mar 2;125(3):1269-85.

Background

AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity), AZD7507 is considered a promising compound as it retained the desired potency and oral pharmacokinetic properties of AZ683. Moreover, in a telemetry study in dogs given a single oral dose, there was no cardiovascular toxicity, no elevation of troponin related to the treatment, and no alteration in the ECG.

Reference

1: Boulter L, Guest RV, Kendall TJ, Wilson DH, Wojtacha D, Robson AJ, Ridgway RA, Samuel K, Van Rooijen N, Barry ST, Wigmore SJ, Sansom OJ, Forbes SJ. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. J Clin Invest. 2015 Mar 2;125(3):1269-85. doi: 10.1172/JCI76452. Epub 2015 Feb 17. PubMed PMID: 25689248; PubMed Central PMCID: PMC4362247.

2: Scott DA, Dakin LA, Daly K, Del Valle DJ, Diebold RB, Drew L, Ezhuthachan J, Gero TW, Ogoe CA, Omer CA, Redmond SP, Repik G, Thakur K, Ye Q, Zheng X. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6. doi: 10.1016/j.bmcl.2013.06.031. Epub 2013 Jun 20. PubMed PMID: 23842474.

Chemical Properties

Cas No. 1041852-85-0 SDF
Chemical Name 4-(2-fluoro-4-methylanilino)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-7-methoxycinnoline-3-carboxamide
Canonical SMILES O=C(C1=NN=C2C=C(OC)C(N3CCN(CCO)CC3)=CC2=C1NC4=CC=C(C)C=C4F)N
Formula C23H27FN6O3 M.Wt 454.51
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2002 mL 11.0009 mL 22.0017 mL
5 mM 0.44 mL 2.2002 mL 4.4003 mL
10 mM 0.22 mL 1.1001 mL 2.2002 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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